OTS964
OTS964 Basic information
- Product Name:
- OTS964
- Synonyms:
-
- OTS964
- (R)-9-[4-[1-(Dimethylamino)propan-2-yl]phenyl]-8-hydroxy-6-methylthieno[2,3-c]quinolin-4(5H)-one Hydrochloride
- (R)-9-(4-(1-(dimethylamino)propan-2-yl)phenyl)-8-hydroxy-6-methylthieno[2,3-c]quinolin-4(5H)-one
- OTS964 HYDROCHLORIDE
- OTS964; OTS 964
- CS-2531
- OTS964 HCl
- OTS964+OTS964 HCl
- CAS:
- 1338545-07-5
- MF:
- C23H24N2O2S
- MW:
- 392.51386
- Product Categories:
-
- API
- Mol File:
- 1338545-07-5.mol
OTS964 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- ≥88.6 mg/mL in DMSO; ≥2.15 mg/mL in EtOH with gentle warming and ultrasonic; ≥2.1 mg/mL in H2O with gentle warming and ultrasonic
- form
- crystalline solid
- color
- Off-white to light yellow
OTS964 Usage And Synthesis
Description
OTS964 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 28 nM). It specifically blocks cytokinesis, leading to apoptosis, in a broad range of cancer cells. OTS964 induces apoptosis of human lung cancer cells in mouse xenografts.
Uses
OTS 964 works through cytokinesis and is an effective TOPK inhibitor which has been shown to cause tumor suppression in xenografts of human cancer.
in vivo
OTS964 hydrochloride (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression[1].
OTS964 hydrochloride (oral administration; 50 or 100 mg/kg/day for 2 weeks) ultimately achieves complete tumor regression[1].
| Animal Model: | Nude mice bearing LU-99 lung cancer cells[1] |
| Dosage: | 40 mg/kg |
| Administration: | Intravenously; on days 1, 4, 8, 11, 15, and 18 |
| Result: | The tumors continued shrinking even after the treatment and finally revealed complete regression. |
| Animal Model: | Nude mice bearing LU-99 lung cancer cells[1] |
| Dosage: | 50 or 100 mg/kg |
| Administration: | Oral administration; once every day for 2 weeks |
| Result: | Achieved complete tumor regression. |
IC 50
TOPK: 28 nM (IC50); CDK11B: 40 nM (Kd)
References
1. matsuo y, park jh2, miyamoto t, et al. topk inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. ci transl med. 2014 oct 22;6(259):259ra145.
OTS964Supplier
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- 0411-62910999 13889544652
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